Gatifloxacin, Uses, Dosage, Side Effects, Interactions, Pregnancy

Gatifloxacin, Uses, Dosage, Side Effects, Interactions, Pregnancy

Gatifloxacin is a synthetic 8-methoxyfluoroquinolone with antibacterial activity against a wide range of gram-negative and gram-positive microorganisms. Gatifloxacin exerts its effect through inhibition of DNA gyrase, an enzyme involved in DNA replication, transcription and repair, and inhibition of topoisomerase IV, an enzyme involved in the partitioning of chromosomal DNA during bacterial cell division.
Gatifloxacin is an antibiotic of the fourth-generation fluoroquinolone family, that like other members of that family, inhibits the bacterial enzymes DNA gyrase and topoisomerase IV. Bristol-Myers Squibb introduced Gatifloxacin in 1999 under the proprietary name Tequin for the treatment of respiratory tract infections, having licensed the medication from Kyorin Pharmaceutical Company of Japan. Allergan produces an eye-drop formulation called Zymar. Gatifloxacin is available as tablets and in various aqueous solutions for intravenous therapy.

Mechanism of Action of Gatifloxacin

Gatifloxacin is a synthetic broad-spectrum 8-methoxyfluoroquinolone antibacterial agent for oral or intravenous administration. is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Gatifloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. It should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.

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The bactericidal action of Gatifloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, and recombination.

Indications of Gatifloxacin

  • Ophthalmic Surgery
  • Conjunctivitis
  • Conjunctivitis, Bacterial
  • For the treatment of bronchitis,
  • Sinusitis,
  • Community-acquired pneumonia,
  • Skin infections (abscesses, wounds) caused by S. pneumoniae, H. influenzae, S. aureus, M. pneumoniae, C. pneumoniae, L. pneumophila, S. pyogenes
  • For the treatment of bronchitis, sinusitis, community-acquired pneumonia, and skin infections (abscesses, wounds) caused by S. pneumoniae, H. influenzae, S. aureus, M. pneumoniae, C. pneumoniae, L. pneumophila, S. pyogenes
  • Infections when due to gatifloxacin-susceptible pathogens: community-acquired pneumonia (mild to moderate) and complicated urinary tract infections (excluding prostatitis and epididymitis.

Contra-Indications of Gatifloxacin

  • History of severe hypersensitivity (e.g. anaphylactic reaction) to any other type of beta-lactam antibacterial agent (penicillins, monobactams, and carbapenems).
  • Hemolytic anemia
  • Liver problems
  • Interstitial nephritis
  • Subacute cutaneous lupus erythematosus
  • Systemic lupus erythematosus
  • use should be avoided in pregnant or lactating women, and in children with developing teeth because they may result in permanent staining (dark yellow-gray teeth with a darker horizontal band that goes across the top and bottom rows of teeth), and possibly affect the growth of teeth and bones.
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Dosage of Gatifloxacin

Strengths: 0.5%; 0.3%

Bacterial Conjunctivitis

0.3% solution

  • Days 1 and 2: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
  • Days 3 through 7: Instill 1 drop in the affected eye(s) up to 4 times a day while awake.

0.5% solution

  • Day 1: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
  • Days 2 through 7: Instill 1 drop in the affected eye(s) 2 to 4 times a day while awake.

Bacterial Conjunctivitis

1 year or older, 0.3% solution

  • Days 1 and 2: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
  • Days 3 through 7: Instill 1 drop in the affected eye(s) up to 4 times a day while awake.

0.5% solution

  • Day 1: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
  • Days 2 through 7: Instill 1 drop in the affected eye(s) 2 to 4 times a day while awake.

Pediatric Bacterial Conjunctivitis

1 year or older; 0.3% solution

  • Days 1 and 2: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
  • Days 3 through 7: Instill 1 drop in the affected eye(s) up to 4 times a day while awake.

0.5% solution

  • Day 1: Instill 1 drop in the affected eye(s) every 2 hours while awake, up to 8 times a day.
  • Days 2 through 7: Instill 1 drop in the affected eye(s) 2 to 4 times a day while awake.

Side Effects of Gatifloxacin

The most common side effects 

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More common

Rare

Drug Interactions of Gatifloxacin

Gatifloxacin may interact with following drugs, supplements, & may change the efficacy of drugs

Pregnancy & Lactation of Gatifloxacin

 FDA Pregnancy Category C

Pregnancy

There are no data available on gatifloxacin ophthalmic use in pregnancy to inform a drug-associated risk. However, animal data have shown that administration of oral gatifloxacin throughout organogenesis and during late gestation through lactation did not produce adverse maternal, fetal, or neonatal effects at clinically relevant doses.

Breastfeeding

There are no data available regarding the presence of gatifloxacin in human milk, the effect of gatifloxacin on breastfeeding infants, or the effect of gatifloxacin on milk production. Animal data have shown that gatifloxacin is excreted in breast milk following oral administration;

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References

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